Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands.

ABSTRACT: Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin ligase have emerged as a novel paradigm in drug development. Herein we found that linker attachment points of CRBN ligands highly affect their aqueous stability and neosubstrate degradation features. This work provides a blueprint for the assembly of future heterodimeric CRBN-based degraders with tailored properties.

SUBMITTER: Bricelj A 

PROVIDER: S-EPMC8591746 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature